AT7867

SKU: orb1300886

Description

AT7867

Research Area

Signal Transduction

Key Properties

• CAS Number: 857531-00-1
• MW: 337.85
• Purity: 99.63%
• Formula: C₂₀H₂₀ClN₃
• SMILES: Clc1ccc(cc1)C1(CCNCC1)c1ccc(cc1)-c1cn[nH]c1
• Target: S6 Kinase,PKA,Akt
• Solubility: DMSO:63 mg/mL (186.47 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:5 mg/mL (14.8 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.96 mM)

Bioactivity

• Target IC50:
  Akt2:17 nM|PKA:20 nM|Akt1:32 nM|p70 S6K:85 nM|Akt3:47 nM
• In Vivo:
  AT7867 shows bioavailability of 44% in mice by p.o. route. AT7867 could increas the cleaved PARP in MES-SA xenografts at 20 mg/kg i.p. or 90 mg/kg p.o. AT7867 significantly inhibit the tumor growth in MES-SA xenografts or U87 mg xenografts with T/C of 0.37 and 0.51, respectively
• In Vitro:
  AT7867 also inhibits structurally related AGC kinases p70S6K and PKA with IC50 of 20 nM and 85 nM, respectively AT7867 shows ATP-competitive activity to Akt2 with Ki of 18 nM. AT7867 exhibits antiproliferation in cell lines with PTEN or PIK3CA mutations and shows great potent to MES-SA, MDA-MB-468, MCF-7, HCT116 and HT29 with IC50 of 0.94 μM, 2.26 μM, 1.86 μM, 1.76 μM and 3.04 μM, respectively AT7867 also suppresse the cell growth of U87 mg, PC-3 and DU145 cells with IC50 of 8.22 μM, 10.37 μM and 11.86 μM, respectively AT7867 suppresses Akt activity by inhibiting phosphorylation of GSK-3β in human tumor cells with IC50 of 2-4 μM. AT7867 also induce the phosphorylation o the following Akt Direct substratees including proapoptotic transcription factors FKHR (FoxO1a), FKHRL1 (FoxO3a) an the downstream target S6RP in U87 mg cells.
• Cell Research:
  Cells are plated in 96-well microplates at 5 × 103 per well in medium supplemented with 10% fetal bovine serum and grown for 24 hours before treatment with AT7867. AT7867 or Vehicle control is added to the cells for 72 hours. Following this, Alamar Blue solution is added the IC50 value for AT7868 is calculated in GraphPad Prism using nonlinear regression analysis and a sigmoidal dose-response (variable slope) equation.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Akt, AT7867, AT-7867, AT 7867, Akt3, Akt2, Akt1, inhibit, Inhibitor, p70 S6K, Protein kinase B, Protein kinase A, Ribosomal S6 Kinase (RSK), S6Kinase, S6K, S6 Kinase, PKB, PKA

Compound Identifiers

PubChem CID

11175137